Reagents and instruments for immunology, cell biology and molecular biology.
 
> Nexturastat A [1403783-31-2]

Nexturastat A [1403783-31-2]

Print Print
Please log in

Cat# HY-16699-10mg

Size : 10mg

Brand : MedChemExpress


Description

Nexturastat A is a potent, selective HDAC6 inhibitor. Nexturastat A has inhibitory for HDAC6 with an IC50 of 5 nM. Nexturastat A can be used for the research of multiple myeloma (MM)[1][2].

IC50 & Target[1]

HDAC6

5.02 nM (IC50)

HDAC8

0.954 μM (IC50)

HDAC1

3.02 μM (IC50)

HDAC7

4.46 μM (IC50)

HDAC11

5.14 μM (IC50)

HDAC3

6.68 μM (IC50)

HDAC9

6.72 μM (IC50)

HDAC2

6.92 μM (IC50)

HDAC10

7.57 μM (IC50)

HDAC4

9.39 μM (IC50)

HDAC5

11.7 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
697 IC50
401 nM
Compound: Nexturastat
Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay
Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay
[PMID: 31710483]
B16 GI50
14.3 μM
Compound: 5g, Nexturastat A
Growth inhibition of mouse B16 cells incubated for 48 hrs by MTT assay
Growth inhibition of mouse B16 cells incubated for 48 hrs by MTT assay
[PMID: 23009203]
MCF7 IC50
1.4 μM
Compound: Nexturastat A
Antiproliferative activity against human MCF7 cells after 48 hrs by CCK-8 assay
Antiproliferative activity against human MCF7 cells after 48 hrs by CCK-8 assay
[PMID: 29317150]
MM1.S IC50
1.76 μM
Compound: Nexturastat
Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
MV4-11 IC50
1.68 μM
Compound: Nexturastat
Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay
[PMID: 34101461]
MV4-11 IC50
1.68 μM
Compound: Nexturastat
Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
Sf9 IC50
0.005 μM
Compound: NextA
Inhibition of recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins followed by s
Inhibition of recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins followed by s
[PMID: 31414801]
Sf9 IC50
2.86 μM
Compound: NextA
Inhibition of recombinant full length C-terminal His/FLAG tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mi
Inhibition of recombinant full length C-terminal His/FLAG tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mi
[PMID: 31414801]
Sf9 IC50
25 nM
Compound: Nexturastat
Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method
Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method
[PMID: 31710483]
Sf9 IC50
3020 nM
Compound: 5g, Nexturastat A
Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate
Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate
[PMID: 23009203]
Sf9 IC50
5.02 nM
Compound: 5g, Nexturastat A
Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate
Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate
[PMID: 23009203]
In Vitro

Nexturastat A (5 g) has inhibitory for HDAC6 with IC50 values of 0.005 μM[1].
Nexturastat A (0-10 μM; 24 h) has substrate selectivity for HDAC62[1].
Nexturastat A has antiproliferative activity against B16 murine melanoma cells with IC50 values of 14.3 μM[1].
Nexturastat A (NexA) (0-40 μM; 48 h) suppresses viability and induced G1 phase arrest of human MM cells[2].
Nexturastat A (0, 30, 40 μM; 48 h) promotes apoptosis of MM cells via transcriptional activation of the p21 promoter[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Nexturastat A Related Antibodies

Western Blot Analysis[1]

Cell Line: B16 murine melanoma cells
Concentration: 0-10 μM
Incubation Time: 24 h
Result: Increased the level of acetyl α-tubulin levels in a dose-dependent.

Cell Viability Assay[2]

Cell Line: RPMI-8226 and U266 cells
Concentration: 0-40 µM
Incubation Time: 48 h
Result: Impaired multiple myeloma (MM) cells viability in a dose- and time-dependent manner.

Apoptosis Analysis[2]

Cell Line: RPMI-8226 and U266 cells
Concentration: 0, 30, 40 μM
Incubation Time: 48 h
Result: Induced cell apoptosis in human MM cells.

RT-PCR[2]

Cell Line: RPMI-8226 and U266 cells
Concentration: 30 µM
Incubation Time: 48 h
Result: Increased the levels of p21 mRNA in RPMI-8226 and U266 cells.
In Vivo

Nexturastat A (NexA) (every two days, 20 days) inhibits tumor growth in murine xenograft models of MM[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

341.40

Formula

C19H23N3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NO)C1=CC=C(CN(CCCC)C(NC2=CC=CC=C2)=O)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 56 mg/mL (164.03 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9291 mL 14.6456 mL 29.2912 mL
5 mM 0.5858 mL 2.9291 mL 5.8582 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Purity & Documentation
References

You might also be interested by the following products:



Cat#
Description
Cond.
Price Bef. VAT
NB-64-08582-10mg
Nexturastat A [1403783-31-2]
 10mg 
NB-64-10891-10mg
U0126 [109511-58-2]
 10mg 
NB-64-24965-10mg
Erdafitinib [1346242-81-6]
 10mg